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Fucoxanthin (FN), a carotenoid derived from brown seaweed and algae, offers significant health benefits. However, its unique structure leads to challenges in stability and bioavailability. To overcome these issues, we successfully encapsulated fucoxanthin in solid lipid nanoparticles (SLNs) utilizing health-safe materials, achieving remarkable results. SLNs exhibited a nanoscale size of 248.98 ± 4.0 nm, along with an impressive encapsulation efficiency of 98.30% ± 0.26% and a loading capacity of 5.48% ± 0.82% in lipid. The polydispersity index (PDI) was measured at 0.161 ± 0.03, indicating a narrow size distribution, while the high negative zeta potential of −32.93 ± 1.2 mV suggests excellent stability. Pharmacokinetic studies conducted in Sprague–Dawley rats revealed an exceptional oral bioavailability of 2723.16% compared to fucoxanthin crystals, likely attributed to the enhanced stability and improved cellular uptake of the SLNs. To further improve bioavailability, we creatively applied enteric coatings to the freeze-dried SLNs, effectively protecting fucoxanthin from gastric degradation, which is supported by in vitro digestion results. These findings underscore the potential of SLNs as a superior delivery system for fucoxanthin, significantly enhancing its therapeutic efficacy and broadening its application in the food and pharmaceutical industries. [ABSTRACT FROM AUTHOR]

Nano-sized biomaterials are innovative drug carriers with nanometric dimensions. Designed with biocompatibility in mind, they enable precise drug delivery while minimizing side effects. Controlled release of therapeutic substances enhances efficacy, opening new possibilities for treating neurological and oncological diseases. Integrated diagnostic-therapeutic nanosystems allow real-time monitoring of treatment effectiveness, which is crucial for therapy personalization. Utilizing biomaterials as nano-sized carriers in conjunction with drugs represents a promising direction that could revolutionize the field of pharmaceutical therapy. Such carriers represent groundbreaking drug delivery systems on a nanometric scale, designed with biocompatibility in mind, enabling precise drug delivery while minimizing side effects. Using biomaterials in synergy with drugs demonstrates significant potential for a revolutionary impact on pharmaceutical therapy. Conclusions drawn from the review indicate that nano-sized biomaterials constitute an innovative tool that can significantly improve therapy effectiveness and safety, especially in treating neurological and oncological diseases. These findings should guide researchers towards further studies to refine nano-sized biomaterials, assess their effectiveness under various pathological conditions, and explore diagnostic-therapeutic applications. Ultimately, these results underscore the promising nature of nano-sized biomaterials as advanced drug carriers, ushering in a new era in nanomedical therapy. [ABSTRACT FROM AUTHOR]

Checkpoint blocking antibodies that interfere in the PD-1/PD-L1 axis provide effective cancer immunotherapy for tumors that are immune inflamed or induced to become "hot". It has also been demonstrated that a small molecule inhibitor of the signaling hub kinase GSK3 can interfere in the PD-1/PD-L1 axis in T-cells by suppressing PD-1 expression. This provides an alternative approach to intervening in the PD-1/PD-L1 axis to provide cancer immunotherapy. In this communication, we demonstrate the remote loading of GSK3 inhibitor AZD1080 into the porous interior of mesoporous silica nanoparticles coated with a lipid bilayer (a.k.a. silicasomes). In a MC38 colon cancer model, intravenous injection (IV) of silicasome-encapsulated AZD1080 significantly improved biodistribution and drug delivery to the tumor site. The improved drug delivery was accompanied by cytotoxic MC38 tumor cell killing by perforin-releasing CD8+ T-cells, exhibiting reduced PD-1 expression. IV injection of encapsulated AZD1080 also resulted in significant tumor shrinkage in other syngeneic mouse tumor models, including another colorectal tumor (CT26), as well as pancreas (KPC) and lung (LLC) cancer models. Not only was the therapeutic efficacy of encapsulated AZD1080 similar or better than anti-PD-1 antibody, but the treatment was devoid of treatment toxicity. These results provide proof-of-principal demonstration of the feasibility of using encapsulated delivery of a GSK3 inhibitor to provide cancer immunotherapy, with the possibility to be used as a monotherapy or in combination with chemotherapy or other immunomodulatory agents.

A nano‐enabled drug delivery acupuncture technology (nd‐Acu) is developed that is based on traditional acupuncture needles where the stainless‐steel surface is designed to deliver various payload molecules. To create the nd‐Acu platform, an electrochemistry procedure is used to attach methyl salicylate‐modified cyclodextrin in which the sugar rings allow the encapsulation of structurally defined single or multiple payload molecules via an inclusion complexation process. Drug loading and release profile are first studied using fluorescent dyes abiotically and at intact animal level. nd‐Acu allows more efficient dye loading and time‐dependent release compared to pristine needles without cyclodextrin modification. Subsequently, a proof‐of‐principle efficacy study is conducted using the platform to load a local anesthetic, lidocaine, for the treatment of knee osteoarthritis (KOA) in mice. It is demonstrated that lidocaine‐laden nd‐Acu can effectively alleviate pain, reduce inflammation, and slow down KOA development biochemically and histologically. Hypothesis‐driven and proteomic approaches are utilized to investigate the working mechanisms of lidocaine nd‐Acu, indicating that the therapeutic outcome is attributed to the in vivo modulation of the HMGB1/TLR4 signaling pathway. The study also obtained preliminary evidence suggesting the involvement of mitochondria as well as small GTPase such as cdc42 during the treatment by lidocaine nd‐Acu. [ABSTRACT FROM AUTHOR]

Abstract A nano‐enabled drug delivery acupuncture technology (nd‐Acu) is developed that is based on traditional acupuncture needles where the stainless‐steel surface is designed to deliver various payload molecules. To create the nd‐Acu platform, an electrochemistry procedure is used to attach methyl salicylate‐modified cyclodextrin in which the sugar rings allow the encapsulation of structurally defined single or multiple payload molecules via an inclusion complexation process. Drug loading and release profile are first studied using fluorescent dyes abiotically and at intact animal level. nd‐Acu allows more efficient dye loading and time‐dependent release compared to pristine needles without cyclodextrin modification. Subsequently, a proof‐of‐principle efficacy study is conducted using the platform to load a local anesthetic, lidocaine, for the treatment of knee osteoarthritis (KOA) in mice. It is demonstrated that lidocaine‐laden nd‐Acu can effectively alleviate pain, reduce inflammation, and slow down KOA development biochemically and histologically. Hypothesis‐driven and proteomic approaches are utilized to investigate the working mechanisms of lidocaine nd‐Acu, indicating that the therapeutic outcome is attributed to the in vivo modulation of the HMGB1/TLR4 signaling pathway. The study also obtained preliminary evidence suggesting the involvement of mitochondria as well as small GTPase such as cdc42 during the treatment by lidocaine nd‐Acu.

[Display omitted] The development of effective therapeutic strategies for triple-negative breast cancer (TNBC), an aggressive subtype with limited treatment options, remains a critical challenge. This study aimed to design and evaluate a combination therapy using chitosan nanoparticles (Cs NPs) loaded with metformin (Met) and methotrexate (MTX) as a promising approach for TNBC management. The Cs NPs exhibited an average size of 78.8 ± 25.84 nm for blank Cs NPs, 84.50 ± 22.54 nm for Met-Cs NPs, and 86.70 ± 30.90 nm for MTX-Cs NPs, with positive surface charges of 26.40 ± 1.40 mV, 28.20 ± 1.60 mV, and 14.30 ± 2.40 mV, respectively. The drug encapsulation efficiency was 88.56 ± 2.26 % for Met-Cs NPs and 97.03 ± 0.52 % for MTX-Cs NPs. The cellular uptake studies demonstrated a time-dependent increase in the accumulation of Shikonin-labeled Cs NPs in 4T1 cells. The cytotoxicity assays revealed that Met-Cs NPs and MTX-Cs NPs exhibited significantly lower IC50 values (19.85 μg/mL and 103.2 ng/mL, respectively) compared to the plain drugs at 48 h. The combination of Met-/MTX-Cs NPs showed a synergistic cytotoxic effect, inducing 50 % cell death at 15.233 μg/mL of Met and 0.166 μg/mL of MTX. In vivo studies using a 4T1 xenograft mouse model demonstrated that the combination of Met-/MTX-Cs NPs resulted in a 100 % reduction in initial tumor volume, compared to a 40 % decrease with the free drug combination. The tumor growth inhibition was 70.45 % for the Met-/MTX-Cs NPs group, significantly higher than the 33.86 % observed in the free drug combination group. The findings of this study highlight the potential of the Met-/MTX-Cs NPs combination as a novel and effective therapeutic approach for TNBC management. The enhanced therapeutic efficacy, improved safety profile, and the ability to modulate key signaling pathways make this nanoparticle-based combination therapy a promising candidate for further clinical investigation. [ABSTRACT FROM AUTHOR]

[Display omitted] • DSPE-PEG2000/DPPC micelles successfully encapsulate the hydrophobic icariin and improve its water solubility. • Aqueous dispersions of ICA-loaded DSPE-PEG2000/DPPC micelles can be atomized well and delivered to the lungs. • DSPE-PEG2000/DPPC micelles can significantly improve the cellular uptake of icariin. Icariin (ICA)-loaded DSPE-PEG2000/DPPC disk-like micelles were synthesized utilizing the thin film hydration method to enhance the solubility and delivery of ICA to the lungs. The micellar formulation significantly improved the water solubility of ICA. This was attributed to the high encapsulation efficiency (95 %) and drug loading capacity (12 %) of the DSPE-PEG2000/DPPC micelles. Comprehensive characterization using Fourier-transform infrared spectroscopy (FT-IR) and X-ray diffraction (XRD). Particle size analysis through dynamic light scattering (DLS) and transmission electron microscopy (TEM) demonstrated the formation of stable micelles with an average particle size around 10 nm. In vitro aerosolization studies using the next-generation impactor (NGI) revealed that the fine particle fraction was 63.5 ± 4 %, which means that over 60 % of the aerosolized ICA/DSPE-PEG2000/DPPC micelles were capable of reaching and targeting the deep lung alveoli, indicating their potential efficacy for pulmonary delivery. Cytotoxicity assessments via the MTT assay showed IC50 values of ICA-loaded DSPE-PEG2000/DPPC micelles were 117 ± 8 μg/mL, 29 ± 3 μg/mL, and 21 ± 1 μg/mL at 24, 48, and 72 h, respectively, highlighting the time-dependent cytotoxic effects of the ICA-loaded micelles on A549 cells. However, the IC50 values of free ICA were > 500 μg/mL, 252 ± 3 μg/mL, and 109 ± 2 μg/mL, respectively at three different time points. That indicated that ICA-loaded nano micelles enhanced the cytotoxicity of ICA. Furthermore, the cellular uptake of the nano micelles by A549 cells was visualized and confirmed using EVOS fluorescence imaging and flow cytometry techniques. In addition, RAW 264.7 M2 polarization studies indicated ICA loaded DSPE-PEG2000/DPPC micelles have potential for treating pulmonary fibrosis. These findings suggest that DSPE-PEG2000/DPPC micelles significantly enhance the solubility and delivery of ICA, presenting a promising nanocarrier system for targeted pulmonary fibrosis therapy. [ABSTRACT FROM AUTHOR]

The skin is essential for body protection and regulating physiological processes. It is the largest organ and serves as the first-line barrier against UV radiation, harmful substances, and infections. Skin cancer is considered the most prevalent type of cancer worldwide, while melanoma skin cancer is having high mortality rates. Skin cancer, including melanoma and non-melanoma forms, is primarily caused by prolonged exposure to UV sunlight and pollution. Currently, treatments for skin cancer include surgery, chemotherapy, and radiotherapy. However, several factors hinder the effectiveness of these treatments, such as low efficacy, the necessity for high concentrations of active components to achieve a therapeutic effect, and poor drug permeation into the stratum corneum or lesions. Additionally, low bioavailability at the target site necessitates high doses, leading to skin irritation and further obstructing drug absorption through the stratum corneum. To overcome these challenges, recent research focuses on developing a medication delivery system based on nanotechnology as an alternative to this traditional approach. Nano-drug delivery systems have demonstrated great promise in treating skin cancer by providing a more effective means of delivering drugs with better stability and drug absorption. An overview of various lipid-based nanocarriers is given in this review article that are utilized to carry natural compounds to treat skin cancer. [Display omitted] [ABSTRACT FROM AUTHOR]

Recent advancements in nanogel formulations have significantly enhanced the therapeutic efficacy of herbal medicines in wound healing applications. This systematic review explores the integration of various herbal extracts and bioactive compounds into nano gels, highlighting their improved properties and wound healing application. Key formulations include tobacco stem nanogels demonstrating stability and rapid wound contraction, neem and silk fibroin hydrogels accelerating wound regeneration, and curcumin nanosuspension-based nanogels significantly enhancing wound contraction rates. Additional formulations, such as Sansevieria trifasciata hydrogels and emodin-based double network hydrogels, showed substantial reductions in wound size and increased cell proliferation. The incorporation of herbal extracts and bioactive compounds like Bletilla striata , curcumin, calendula, and Hibiscus rosa-sinensis further exhibited enhanced coagulation, antioxidant effects, and fibroblast proliferation. This review highlights the promising future of herbal nanogels in biomedical applications, offering a synergistic approach that combines the benefits of traditional herbal medicine with advanced nanotechnology.

Objective: In the treatment of severe cases of bacterial keratitis, conventional eye drops containing antibiotics should be applied daily and very frequently. The aim of this study is to develop low-dose high-effect formulations with the prepared nanostructured lipid carrier (NLC) formulations to reduce antibiotic resistance and increase patient compliance. Methods: NLC formulations were loaded with besifloxacin HCl (BHL) and the besifloxacin HCl: sulfobutyl ether beta-cyclodextrin (SBE-CD) complex. Positive charge was gained with chitosan, and corneal permeation and resolubility were increased with SBE-CD. In vitro characterization studies, permeability studies, and cytotoxicity and ex vivo transport studies were carried out. Results: In this study, it was found that SBE-CD increased BHL's solubility by 8-fold based on phase solubility studies. The optimized NLCs were small in size (13.63-16.09 nm) with a low polydispersity index (0.107-0.181) and adequate BHL drug loading efficiency. In vitro release studies showed that formulations were released approximately for 8 h and at levels over the minimum inhibitory concentration of Pseudomonas aeruginosa and Staphylococcus aureus. NLC formulations had a better corneal permeation rate than the marketed product during 6 h of ex vivo studies. Conclusions: According to in vitro and ex vivo data, it was determined that the most favorable NLC formulation was the formulation containing BHL/SBE-CD that was covered with chitosan. It has the highest drug loading capacity and one of the highest ex vivo corneal passage levels, along with desired drug release. The formulation containing BHL/SBE-CD and chitosan can be a potential alternative for the treatment of bacterial keratitis. [ABSTRACT FROM AUTHOR]

Background: Following the COVID-19 pandemic, microvascular and macrovascular thrombotic problems emerged that required anticoagulants. Apixaban (RN) is a factor Xa inhibitor that treats deep vein thrombosis and the two forms of artery diseases (coronary artery disease and peripheral artery disease)., Materials and Methods: The study objective was to create fast-disintegrating Apixaban Oral Thin Films (OTF) with the help of various super disintegrants to shorten disintegration time and enhance drug release in order to assist patients who have difficulty in swallowing conventional dosage forms and increase bioavailability. OTF was created using the solvent casting method. A 22 factorial design was employed in Design-Expert® software to develop an ideal formula., Results: The optimized film formula pH, drug content, disintegration time, folding endurance, and dissolution rate were estimated, and the film was subjected to a short-term stability study. The optimized formula exhibited a cumulative drug release of 93.47% in 60 sec., Conclusion: The drug's in vitro release pattern shows first-order kinetics and fickian diffusion was the mechanism of drug release. These findings supported that Apixaban OTFs offer a quick release of the medication from the administration site into the systemic circulation.

Background and Objectives: Nanosponges are one of the most innovative ways to use the newest developments in nanodrugs delivery. Nanosponges can catch drugs that dissolve in water or ones that don't. This work uses statistical design to find the best nanosponges for drugs that don't dissolve easily and make them., Material and Methods: It was looked into how to statistically make the most of the effects of independent factors. The ethyl cellulose ratio and stirring rate were chosen based on how they affected the dependent variables, such as particle size and how well they were trapped. FTIR, SEM, zeta potential, entrapment efficiency, and particle size data were used to test the nanosponges that were made. Using carbopol, the best lot of nanosponges was added to the gel., Results: Using ethyl cellulose and polyvinyl alcohol as stabilizers in the emulsion liquid diffusion method, it was possible to make drug-loaded nanosponges. It was possible to make the nanosponges composition work better by using Central Composite Design. It has been seen that making drug-filled nanosponges improves stability., Conclusion: The study showcased the enhanced capacity of a formulation with decreased particle size and high entrapment efficiency to disseminate effectively.

Introduction: Radiation - induced damage to the hematopoietic and gastrointestinal system especially intestine is a major concern for individuals exposed to ionizing radiation. Resveratrol has shown potential in mitigating radiation - induced toxicity, but its efficacy may be limited by its low bioavailability. In this study, we aimed to evaluate the effectiveness of resveratrol - loaded polymeric - based nanocapsules in mitigating radiation - induced injury to the hematopoietic system and intestine after whole - body exposure to X-ray radiation in NMRI mice. Methods: Sixty male NMRI mice were randomly divided into four groups: control, radiation, resveratrol only, and resveratrol+radiation. Mice were exposed to a single dose of 7.2 Gy of X-ray radiation. Resveratrol - loaded polymeric - based nanocapsules were administered to the mice in the sham and resveratrol treatment groups through gavage. Mice were sacrificed on day 7 post - irradiation, and blood and tissue samples were collected for CBC, histopathological and biochemical evaluation. Results: The study found that resveratrol - loaded polymeric - based nanocapsules effectively (significantly) mitigated radiation - induced injury to the hematopoietic system and intestine. The histopathological evaluation showed a slight decrease (non - significant) in goblet cell injury, villi shortening, inflammation, and mucous layer thickness in the resveratrol treatment group compared to the radiation group. Biochemical evaluation showed a significant increase in GPx and SOD activities in the resveratrol treatment group compared to the radiation group. Resveratrol treatment group showed a significant improvement in some of blood parameters compared to the radiation group. Conclusions: The findings suggest that resveratrol - loaded polymeric - based nanocapsules can be an effective approach to mitigate radiation - induced damage to the hematopoietic system and intestine after whole - body exposure to X-ray radiation in mice. Further research is needed to explore the optimal dose and timing of resveratrol administration and to investigate the potential for clinical translation of this approach. [ABSTRACT FROM AUTHOR]

[Display omitted] • The FeC 22 nanocage was assessed for the formation of ALP@FeC 22 conjugations. • The O...Fe, N...Fe, and H...C interactions were found. • The N...Fe and H...C interactions yielded the strongest ALP@FeC 22 conjugation. • The HOMO-LUMO features indicated a significant role of FeC 22 for the conjugation. • The employed FeC 22 nanocage was proposed as a possible carrier of ALP drug. An iron-doped nanocage (FeC 22) was assessed in this work based on density functional theory (DFT) calculations to work as a carrier of allopurinol (ALP) drug during its adsorption. The structural and electronic specifications were evaluated to analyze the formation of ALP@FeC 22 conjugation yielding A1, A2, and A3 configurations with different featured properties. The existences of O...Fe, N...Fe, and H...C interactions were found for the conjugation formation in a physical non-covalent mode, in which the collaboration of N...Fe and H...C interactions yielded the strongest A3 conjugation with −49.31 kcal/mol strength. Interactions details also confirmed the formation of such strong conjugation. The electronic specifications based on the dominant frontier molecular orbitals showed measurable variations of features from the parental nanocage to the conjugation and also among the configurations. Finally, the FeC 22 nanocage was proposed as a possible carrier of ALP by the formation of ALP@FeC 22 conjugation for a smart drug delivery platform. [ABSTRACT FROM AUTHOR]

Abdel-Majeed Safer,1 Stefano Leporatti,2 Jacquilion Jose,3 Mahmoud S Soliman4 1Department of Biological Sciences, Faculty of Science, Kuwait University, Kuwait City, Kuwait; 2CNR Nanotec, Istituto di Nanotecnologia, Lecce 73100, Italy; 3Nanoscopy Science Center, Faculty of Science, Kuwait University, Kuwait City, Kuwait; 4Nanotechnology Research Facility, Faculty of Engineering and Petroleum, College of Engineering and Petroleum, Kuwait University, Kuwait City, KuwaitCorrespondence: Abdel-Majeed SaferDepartment of Biological Sciences, Faculty of Science, Kuwait University, Kuwait City, KuwaitTel +965 2 498 5909Email saferam52@gmail.com Stefano LeporattiCNR Nanotec, Istituto di Nanotecnologia, Lecce, ItalyTel +39 0832 319 829Email stefano.leporatti@nanotec.cnr.itPurpose: Chitosan nanoparticles (CS NPs) have been used as a good vehicle for nano-drug delivery due to their good physicochemical properties. Epigallocatechin-3-gallate (EGCG), one of the major active ingredients of green tea, is a natural antioxidant that helps in reducing and preventing cell damage and fighting cancer, plus providing other benefits. The aim of this study is to optimise the preparation parameters in terms of the physical characteristics and stability in CS/EGCG NPs conjugation.Results: The conjugation of CS/EGCGNPs was obtained by means of Poloxamer 188. The average CS/EGCG NPs complex was of size 117.8±38.71nm with a surface charge of +67.8±4.38mV and isoelectric point at pH 7.61.Conclusion: In conclusion, NPs produced were stable at 4°C with nanometric size, good polydispersity, good loading and efficiency, envisaging to be a possible candidate for nano-therapeutic delivery system against hepatic fibrosis.Keywords: chitosan, EGCG, conjugation, nano-drug delivery

Mona Ebadi,1 Bullo Saifullah,1,2 Kalaivani Buskaran,2 Mohd Zobir Hussein,1 Sharida Fakurazi31Materials Synthesis and Characterization Laboratory, Institute of Advanced Technology (ITMA), Universiti Putra Malaysia, Serdang, Selangor 43400, Malaysia; 2Laboratory for Vaccine and Immunotherapeutic, Institute of Biosciences, Universiti Putra Malaysia, Serdang, Selangor 43400, Malaysia; 3Department of Human Anatomy, Faculty of Medicine and Health Sciences, Universiti Putra Malaysia, Serdang, Selangor 43400, MalaysiaCorrespondence: Mohd Zobir HusseinMaterials Synthesis and Characterization Laboratory, Institute of Advanced Technology (ITMA), Universiti Putra Malaysia, Serdang, Selangor 43400, MalaysiaTel +60 38 946 8092Email mzobir@upm.edu.myBackground: Cancer treatments are being continually developed. Increasingly more effective and better-targeted treatments are available. As treatment has developed, the outcomes have improved.Purpose: In this work, polyethylene glycol (PEG), layered double hydroxide (LDH) and 5-fluorouracil (5-FU) were used as a stabilizing agent, a carrier and an anticancer active agent, respectively.Characterization and methods: Magnetite nanoparticles (Fe3O4) coated with polyethylene glycol (PEG) and co-coated with 5-fluorouracil/Mg/Al- or Zn/Al-layered double hydroxide were synthesized by co-precipitation technique. Structural, magnetic properties, particle shape, particle size and drug loading percentage of the magnetic nanoparticles were investigated by XRD, TGA, FTIR, DLS, FESEM, TEM, VSM, UV-vis spectroscopy and HPLC techniques.Results: XRD, TGA and FTIR studies confirmed the formation of Fe3O4 phase and the presence of iron oxide nanoparticles, polyethylene glycol, LDH and the drug for all the synthesized samples. The size of the nanoparticles co-coated with Mg/Al-LDH is about 27 nm compared to 40 nm when they were co-coated with Zn/Al-LDH, with both showings near uniform spherical shape. The iron oxide nanoparticles retain their superparamagnetic property when they were coated with polyethylene glycol, polyethylene glycol co-coated with Mg/Al-LDH and polyethylene glycol co-coated with Zn/Al-LDH with magnetic saturation value of 56, 40 and 27 emu/g, respectively. The cytotoxicity study reveals that the anticancer nanodelivery system has better anticancer activity than the free drug, 5-FU against liver cancer HepG2 cells and at the same time, it was found to be less toxic to the normal fibroblast 3T3 cells.Conclusion: These are unique core-shell nanoparticles synthesized with the presence of multiple functionalities are hoped can be used as a multifunctional nanocarrier with the capability of targeted delivery using an external magnetic field and can also be exploited as hypothermia for cancer cells in addition to the chemotherapy property.Keywords: nano drug delivery, layered double hydroxide, core-shell nanoparticles, iron oxide nanoparticles, 5-fluorouracil

One of the most common malignancies in women, breast cancer accounts for nearly 25% of all cancer cases. Breast cancer is a diverse cancer form that exhibits variability in both morphology and molecular characteristics, and is linked to numerous risk factors. Although various approaches and research are ongoing in the treatment and prevention of breast cancer, medication resistance in the current breast cancer treatment contributes to the disease's relapse and recurrence. Phytoactive molecules are the subject of growing research in both breast cancer prevention and treatment but currently used conventional medicines and techniques limit their application. Recent years have seen significant advancements in the field of nanotechnology, which has proven to be essential in the fight against drug resistance. The transport of synthetic and natural anticancer molecules via nanocarriers has recently been added to breast cancer therapy, greatly alleviating the constraints of the current approach. In light of these developments, interest in nano-delivery studies of phytoactive molecules has also increased. In this review, research of phytoactive molecules for breast cancers along with their clinical studies and nanoformulations, was presented from current and future perspectives., (Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.net.)

Utilization of unique acidic environment in various disease sites has been quite advantageous in targeted drug delivery. Among the widely explored pH-sensitive moieties such as hydrazone, orthoester, imine, vinylether, etc. , the acetal bearing compounds are one of the most explored entities in targeted and improved drug delivery to treat disease conditions at the preclinical stage. This review addresses the design and synthesis of various acetal-based polymers as pH-responsive nano-drug delivery systems in the form of micelles, polymersomes, nanoplexes and polymeric and solid lipid nanoparticles for biomedical applications. The review will identify potential advantages, key challenges and future prospects of acetal-based pH-responsive drug delivery systems. The novel developments, strategies and suggestions described may guide the formulation scientists to optimize acetal-based pH-responsive drug delivery systems as an approach to treat various diseases. Unlabelled Image • Acetals hydrolyse at acidic pH following a first order kinetics. • Benzylidene acetal containing amphiphilic polymers self-assemble into nano-systems. • Acetal-based nano-systems facilitate targeted drug delivery in response to low pH. • The approach shows promising applications to treat cancer and bacterial infections. [ABSTRACT FROM AUTHOR]

Hepatoprotective effects of many antioxidants have been attributed with its uncertain bioavailability at the target cell. Research in drug delivery today is to design a nano-carrier system to deliver drugs at target cell with desired dose and duration. In this study, sodium alginate coated catechin nanoparticle (SACC-NP) carrier system was evaluated for its in vivo anti-oxidant potential in rat model revealed improvement in hematological, biochemical parameters and oxidative stress markers on day 28th of SACC-NPs treated group of rats (Gr. V). Significant improvement in healing pattern of liver along with regenerative changes during histopathology studies was observed in the rats of Gr. V. Results of gross pathology and histopathology with the liver of rats receiving SACC-NPs has been re-confirmed again by May-Grunwald Giemsa staining which recorded prominent regenerative changes in liver. Modified scoring pattern also re-ascertained regenerative changes in the liver tissue of the rats receiving SACC-NPs. [ABSTRACT FROM AUTHOR]

G protein-coupled receptor (GPCR) 87, is overexpressed in various cancer cells especially pancreatic cancer and plays a critical role in tumor cell survival. Nano-particles (NP) have become the essential vehicles for nucleotide internalization to the cell, due to the negative charge of nucleotides and their poor stability in blood circulation. In this study, the HEK293T cell linewas transfected with GPR87-plasmid after which the double-stranded RNA molecules targeting the GPR87 gene were prepared and purified. 1.1B4 cancer cell lines were used as model pancreatic cancer cells. Produced siRNA molecules were encapsulated in Poly(Lactic-Co-Glycolic Acid) (PLGA) nano-micelles using three different methods, two of which were according to literature with (siR-PLGA-S) or without (siR-PLGA-V) sonication. However, a new method was suggested to overcome problems such as poly-dispersity and large sizes of siR-PLGA-S and siR-PLGA-V. The new method consists of encapsulating siRNA using mild agitation to the pre-made PLGA NPs. The latter method provided mono-dispersed particles (siR-P-PLGA) with 92 nm size and desired Encapsulation Efficiency (EE%). siR-P-PLGA was able to silence the GPR-87 gene in a ratio of 83.9%, almost 41 times more effective than siR-PLGA-S and siR-PLGA-V in HEK 293 T cells. siR-P-PLGA was able to show a mild cytotoxic effect on 1.1B4 pancreatic cancer cells within 48 h. [ABSTRACT FROM AUTHOR]

[Display omitted] • A complete introduction to metal drugs and probes based on micelles, liposomes, nanoparticles, nanosheets, metal-phenolic networks, and metal–organic frameworks. • Metal-based compounds as drugs, drug delivery systems, fluorescent probes, MRI contrast agents, and other diagnostic imaging probes for tumors. • Analysis and solutions for toxicity of metal nanosystems. • Clinical applications of metal drugs and probes, analysis of the reasons for difficulties in clinical translation, and presentation of future perspectives. Tumors, particularly malignant ones, seriously impact human health. Numerous studies have demonstrated the exceptional potential of metal-based nanosystems, both as drugs and drug delivery systems (DDS), in killing tumor cells in combination with chemotherapy, phototherapy, immunotherapy, radiotherapy, and other treatments, resulting in considerable therapeutic effects against tumors. Furthermore, metal-based fluorescent probes can diagnose tumors by detecting tumor-related biomarkers, and contrast agents (CAs) can diagnose tumors by contrasting imaging between normal and tumor tissues. These two types of diagnostic probes play a critical role in tumor prevention and monitoring of clinical treatment effects. This review focuses on recent advances in metal-based micelles, liposomes, nanoparticles (NPs), nanosheets (NSs), metal-phenolic networks (MPNs), and metal-organic frameworks (MOFs) nanosystems, as well as their applications as drugs, DDS, and probes over the past five years. This review also highlights the latest research advances in their use as fluorescence diagnostic probes and magnetic resonance imaging (MRI) CAs in tumors. Furthermore, the toxicity mechanism of metal-based nanosystems is analyzed, and the strategies to reduce their systemic toxicity are proposed. Finally, this review includes a conclusion and a prospect for the future clinical translation of metal-based nanosystems in the diagnosis and treatment of tumors. [ABSTRACT FROM AUTHOR]

Colorectal cancer (CRC) is the leading cause of cancer-related mortality, annually responsible for around 655,000 deaths worldwide. CRC usually develops very slowly, over a period of 10 to 20 years and typically begin as a non-cancerous polyp that develops on the inner layer of the colon or rectum. However, CRC is curable if detected at an early stage. The current treatment of colorectal cancer primarily depends on surgery, chemotherapy, radiotherapy and targeted therapy. A combination of two or more treatments is often recommended to achieve the best outcome, depending on the stage of cancer development. In this review, we summarized the challenges of using 5-Fluorouracil as chemotherapy to treat colorectal cancer, and discussed the implications of nano drug delivery system for improved therapeutic outcome of 5-Flurouracil.

Chirality, one of the most fundamental properties of natural molecules, plays a significant role in biochemical reactions. Nanomaterials with chiral characteristics have superior properties, such as catalytic properties, optoelectronic properties, and photothermal properties, which have significant potential for specific applications in nanomedicine. Biomolecular modifications such as nucleic acids, peptides, proteins, and polysaccharides are sources of chirality for nanomaterials with great potential for application in addition to intrinsic chirality, artificial macromolecules, and metals. Two-dimensional (2D) nanomaterials, as opposed to other dimensions, due to proper surface area, extensive modification sites, drug loading potential, and simplicity of preparation, are prepared and utilized in diagnostic applications, drug delivery research, and tumor therapy. Current advanced studies on 2D chiral nanomaterials for biomedicine are focused on novel chiral development, structural control, and materials sustainability applications. However, despite the advances in biomedical research, chiral 2D nanomaterials still confront challenges such as the difficulty of synthesis, quality control, batch preparation, chiral stability, and chiral recognition and selectivity. This review aims to provide a comprehensive overview of the origins, synthesis, applications, and challenges of 2D chiral nanomaterials with biomolecules as cargo and chiral modifications and highlight their potential roles in biomedicine.

The blood–brain barrier (BBB) plays a vital role in the protection and maintenance of homeostasis in the brain. In this way, it is an interesting target as an interface for various types of drug delivery, specifically in the context of the treatment of several neuropathological conditions where the therapeutic agents cannot cross the BBB. Drug toxicity and on-target specificity are among some of the limitations associated with current neurotherapeutics. In recent years, advances in nanodrug delivery have enabled the carrier system containing the active therapeutic drug to target the signaling pathways and pathophysiology that are closely linked to central nervous system (CNS) disorders such as Alzheimer’s disease (AD), Parkinson’s disease (PD), Huntington’s disease (HD), multiple sclerosis (MS), brain tumor, epilepsy, ischemic stroke, and neurodegeneration. At present, among the nano formulations, solid lipid nanoparticles (SLNs) have emerged as a putative drug carrier system that can deliver the active therapeutics (drug-loaded SLNs) across the BBB at the target site of the brain, offering a novel approach with controlled drug delivery, longer circulation time, target specificity, and higher efficacy, and more importantly, reducing toxicity in a biomimetic way. This paper highlights the synthesis and application of SLNs as a novel nontoxic formulation strategy to carry CNS drugs across the BBB to improve the use of therapeutics agents in treating major neurological disorders in future clinics.

Visceral leishmaniasis (VL) is a life-threatening parasitic disease affecting impoverished people of the developing world; and much effort has been spent on the early case detection and treatment. However, current diagnostics and treatment options are not sufficient for appropriate surveillance in VL elimination setting. Hence, there is a dire need to develop highly sensitive diagnostics and less toxic effective treatments for proper management of cases and to achieve the sustained disease elimination. Although, promising results have been observed with nanomedicines in leishmaniasis; there are great challenges ahead especially in translating this to clinical setting. This review provides updated progress of nanomedicines in VL, and discussed how these innovations and future directions play vital role in achieving VL elimination. [ABSTRACT FROM AUTHOR]

controlled drug is a process where a carrier has an account with medication can be combined to form the active drug in the body operating the preset desired from this article be abandoned and, therefore, the optimization of the release drug is of special importance. In the present study, Curcumin drug release based on statistical methods that include response surface curve and the method of multivariate modeling can be hard to check, and then optimize the results of drug release both methods can be compared and demonstrated that although the model obtained from the level of responses to experimental, but because the taking effect of the invoices is capable of simultaneously the amount of drug in release Effective factor values that measure has not yet been done as well as anticipated. In addition it's possible to calculate the effect of each factor and higher power in the process of release reviewed.

Abstract Current drug therapy against infections is threatening to become obsolete due to the poor physical, chemical, biological and pharmacokinetic properties of drugs, followed by high risk of acquiring resistance. Taking into account the significant benefits of nanotechnology, nano-based delivery of anti-infectious agents is emerging as a potential approach to combat several lethal infections. Co-delivery of multiple anti-infectious agents in a single nano-based system is beginning to show significant advantages over mono-therapy, such as synergism, enhanced anti-microbial activity, broad anti-microbial spectrum, reduced resistance development, and improved and cost-effective treatment. The current review provides a detailed update on the status of various lipid and polymer based nano-systems used to co-deliver multiple anti-infectious agents against bacterial, HIV and malarial infections. It also identifies current key challenges and suggests strategies to overcome them, thus guiding formulation scientists to further optimize nano-based co-drug delivery as an approach to fight infections effectively. Graphical abstract Unlabelled Image [ABSTRACT FROM AUTHOR]

Stimuli-responsive polymeric drug delivery systems using various triggers to release the drug at the sites have become a major focus area. Among various stimuli-responsive materials, pH-responsiveness has been studied extensively. The materials used for fabricating pH-responsive drug delivery systems include a specific chemical functionality in their structure that can respond to changes in the pH of the surrounding environment. Various chemical functionalities, for example, acetal, amine, ortho ester, amine and hydrazone, have been used to design materials that are capable of releasing their payload at the acidic pH conditions of the tumor or infection sites. Hydrazone linkages are significant synthons for numerous transformations and have gained importance in pharmaceutical sciences due to their various biological and clinical applications. These linkages have been employed in various drug delivery vehicles, such as linear polymers, star shaped polymers, dendrimers, micelles, liposomes and inorganic nanoparticles, for pH-responsive drug delivery. This review paper focuses on the synthesis and characterization methods of hydrazone bond containing materials and their applications in pH-responsive drug delivery systems. It provides detailed suggestions as guidelines to materials and formulation scientists for designing biocompatible pH-responsive materials with hydrazone linkages and identifying future studies. [ABSTRACT FROM AUTHOR]

Since the late 1990s, there has been rapid multiplication of data on the anti-cancer properties of artemisinins. This article reviews the status of progress of artemisinin and its derivatives as anti-cancer agents in clinical trials, case reports, and in vitro/in vivo studies. Particular attention is laid on the combinations of artemisinins and synthetic chemodrugs to enhance the latter's efficacy. An attempt is here made to rationalize the synergistic effects of a few common anti-cancer drugs of the anthracycline, taxane, anti-metabolite, and platinum-based drug families. The various pathways that mediate the action of artemisinins as reported over the past decade are here summarized highlighting also the biomarkers that could be used to better predict the efficacy of the sesquiterpenoids. Their main action seems to be directed toward stalling tumor cell proliferation through cell cycle arrest mediated by reactive oxygen species (ROS). The emergence of artemisinins' nano-based formulations in combination with chemodrugs to enhance drug bioavailability and targeting as well as immunotherapy is also reviewed. The enhanced efficacy of artemisinin dimers compared to the parent molecules and standard chemotherapy is analyzed. While these therapies hold promises, it may be premature to conclude on their efficacy in the absence of clinical studies. [ABSTRACT FROM AUTHOR]

This work was carried out by the importance of providing insights into the nano-based drug delivery of anticancers. To this aim, a representative model of aluminum nitride (AN) nanocage scaffold and two of its boron and gallium doped forms (BAN and GAN) were investigated towards the adsorption of thiotepa (Tep) anticancer. Density functional theory (DFT) calculations were performed to evaluate the stabilized structures and their corresponding electronic features. The results indicated the contribution of N-head and S-head of Tep to interactions with each scaffold resulting six complexes; NTep@AN and STep@AN, NTep@BAN and STep@BAN, NTep@GAN and STep@GAN. In each complex model, the characteristic features were obtained based on the interactions details and frontier molecular orbitals related features. In this regard, the investigated scaffolds were found suitable for adsorbing the Tep substance with different strengths and frontier molecular orbitals levels yielding the possibility of assigning specified recovery time and conductance. As a consequence, the models of investigated scaffolds were found suitable to work as possible carriers of Tep anticancer for approaching the nano-based drug delivery purposes. [Display omitted] • Structural and electronic features showed the possibility Tep@Scaffold formations. • N-head and S-head of Tep were involved in interactions with the scaffolds. • NTep@BAN was the strongest complex and STep@BAN was the weakest one. • The recovery time and frontier molecular orbitals indicated different conductance rates. • AN, BAN, and GAN scaffolds were found suitable for adsorbing the Tep substance. [ABSTRACT FROM AUTHOR]

Objective: Addressing both the initial treatment response and subsequent paclitaxel resistance is a pivotal concern. Nano drug delivery, an emerging approach, presents a cutting-edge alternative to conventional chemotherapy., Methods: This investigation synthesized PEGylated nanoparticles (NPs) via the Reverse Phase Evaporation technique for liposomal NPs. Characteristics such as zeta potential, size, drug release and polydispersity index (PDI) were subjected to evaluation. Subsequently, cytotoxicity assays were conducted on gastric cancer cells (AGS) following 24 and 48-hour incubation periods., Results: In this study, the liposomal NPs had a zeta potential of -22 mV and a particle size of 285 nm. The Entrapment efficiency was determined as 41% that occurred physically. Additionally, the liposomal NPs demonstrated a high drug retention rate (39% remained after 72 hours), and they exhibited significantly increased cytotoxicity compared to the free drug, confirming their effectiveness as a suitable carrier for paclitaxel during both incubation periods (P<0.05)., Conclusion: These findings collectively advocate the potential of liposomal NPs as promising contenders for effective nano-drug application in propelling chemotherapy forward.